Janus kinase 3 inhibitors, also called JAK3 inhibitors, are a new class of immunomodulatory agents that inhibit Janus kinase 3. They are used for the treatment of autoimmune diseases. …

The design of new JAK3 covalent inhibitors could be supported by the success of ritlecitinib in reaching the clinical trial (NCT04517864). In addition, advances in X-ray and covalent docking …

2022年8月19日 · Here, a highly JAK3-selective inhibitor Z583 is developed, which showed a potent inhibition of JAK3 with an IC 50 of 0.1 nM and exhibited a 4500-fold selectivity for JAK3 …

2018年3月27日 · In this paper, we describe a newly discovered irreversible covalent JAK3 inhibitor RB1, which exhibits higher JAK isoform selectivity for JAK3 and shows suitable …

Decernotinib is reported to be a JAK3-selective inhibitor developed to preserve JAK1 and JAK2 signaling, which, in principle, would eliminate non-immunologic adverse effects. This is …

2016年10月28日 · PF-06651600, a newly discovered potent JAK3-selective inhibitor, is highly efficacious at inhibiting γc cytokine signaling, which is dependent on both JAK1 and JAK3. PF …

A Janus kinase inhibitor, also known as JAK inhibitor or jakinib, [1] is a type of immune modulating medication, which inhibits the activity of one or more of the Janus kinase family of enzymes …

2023年12月20日 · The JAK3 inhibitor reduces ILC2 survival, proliferation, and cytokine production in vitro and ameliorates ILC2-driven Alternaria-induced asthma. Furthermore, combining a …

Janus kinase inhibitors (JAKis) represent a fundamental therapeutic tool for the treatment of patients with immune-mediated inflammatory diseases. Although JAKis are often considered a …

Selective inhibition of Janus kinase 3 (JAK3) is a promising strategy for the treatment of autoimmune diseases. Based on the discovery of a hydrophobic pocket unutilized between the …